[18F]fluoromethylbenzylsulfonate ester: a rapid and efficient synthetic method for the N-[18F]fluoromethylbenzylation of amides and amines.
We have prepared 4-[18F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [18F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[18F]fluoromethylbenzylsulfonate esters to N-alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[18F]fluoromethylbenzyl)spiperone and 1-N-(4-[18F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.
Choe
Y S
YS
Department of Nuclear Medicine, Samsung Medical Center, Seoul, South Korea.
Song
D H
DH
Lee
K J
KJ
Kim
S E
SE
Choi
Y
Y
Lee
K H
KH
Kim
B T
BT
Oh
S J
SJ
Chi
D Y
DY
D000477:Alkylating Agents / Q000737:chemistry; D000478:Alkylation; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D008698:Mesylates / Q000737:chemistry*; D010879:Piperazines / Q000737:chemistry; D013134:Spiperone / Q000737:chemistry
C110737:18F-fluoromethylbenzylsulfonate ester; D000477:Alkylating Agents; D005462:Fluorine Radioisotopes; D008698:Mesylates; D010879:Piperazines; D013134:Spiperone; C031503:phenylpiperazine